In situ gastric floating gel of atazanavir sulphate for sustained release: formulation, optimization and evaluation.

IF 3 Q2 PHARMACOLOGY & PHARMACY Therapeutic delivery Pub Date : 2023-10-01 Epub Date: 2023-12-06 DOI:10.4155/tde-2023-0037
Rajashree Masareddy, Pradnya Sandure, Archana Patil, Yadishma Gaude, Arpana Patil
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Abstract

Aim: Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. Materials & methods: The in situ floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 32 full factorial design. Results: Floating lag time of optimized formulation was found to be 18 s and percentage drug release of 94.18 ± 0.18 % at the end of 16 h. The concentration of gelling polymer affects drug release and a floating lag time and vice versa. Conclusion: In situ floating gel of atazanavir sulphate was found promising to sustain drug release due to an increased gastric residence time, which leads to enhanced potential therapy.

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用于持续释放的硫酸阿扎那韦原位胃漂浮凝胶:配方、优化和评估。
目的:硫酸阿扎那韦属 BCS II 类药物,由于其快速的首过代谢和 P-gp 外流,其口服生物利用度有限。材料与方法:采用离子凝胶法制备了使用复方药物的原位浮动凝胶,并按照 32 全因子设计优化了配方。结果:胶凝聚合物的浓度会影响药物释放和浮滞时间,反之亦然。结论硫酸阿扎那韦原位浮动凝胶由于增加了胃停留时间而有望持续释放药物,从而提高了潜在治疗效果。
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来源期刊
Therapeutic delivery
Therapeutic delivery PHARMACOLOGY & PHARMACY-
CiteScore
5.50
自引率
0.00%
发文量
25
期刊介绍: Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.
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